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BroadPharm技术讲座-What is SM-102?

更新时间:2023-09-08   点击次数:270次

中文介绍:

脂质纳米颗粒最近开始流行,作为mRNA疫苗和疾病治疗的有效递送载体。其中一种更值得注意的脂质是可电离脂质 SM-102,用于配制疫苗 mRNA-1273 - 由 Moderna 获得。

SM-102是一种氨基脂质,具有叔胺和通过酯键连接的支尾。叔胺允许脂质形成两性离子脂质。SM-102是一种无色油性化合物,分子量为710.2,CAS号为2089251-47-6。IUPAC的名称是庚烷-9-基8-[2-乙基-(6-氧代-6-十一氧基己基)氨基]辛酸酯。

SM-102因其快速清除率、耐受性、免疫原性和蛋白表达而成为理想的药物载体。虽然SM-102可溶于有机溶剂,但悬浮在极性溶剂中时会形成膜。这一特性使科学家能够将这些脂质塑造成mRNA疗法。SM-102在mRNA-1273的配制中起重要作用。SM-102在生理pH下保持中性,并在酸性环境中带正电荷。这种在生理pH下保持中性的特性允许脂质与血细胞阴离子膜的相互作用更少。SM-102带正电荷的能力在细胞摄取后起着至关重要的作用。当SM-102与酸性内体相互作用时,它变得质子化并形成锥形离子对,驱动从双层到倒六边形相的转变。这个阶段促进内体逃逸和mRNA释放到细胞质中。一旦mRNA被释放,SM-102通过酯水解代谢,剩余的脂肪族头基通过胆道和肾脏清除被消除。

随着脂质技术的最新进展,科学界正处于创造许多新疗法的边缘。为了进一步增强药物递送研究的能力,BroadPharm(国内客户联系靶点科技)提供了广泛的可电离脂质、阳离子脂质、PEG 脂质和磷脂选择。BroadPharm(国内客户联系靶点科技)还提供定制的脂质合成,以满足您的研究需求。


英文介绍:

Lipid nanoparticles have recently come into vogue as an effective delivery vehicle for mRNA vaccines and disease treatment. One of the more notable lipids is the ionizable lipid SM-102, used in the formulation of the  vaccine mRNA-1273 - patented by Moderna.


SM-102 is an amino lipid with a tertiary amine and a branched tail linked through ester bonds. The tertiary amine allows the lipid to form a zwitterionic lipid. SM-102 is a colorless oily compound with a molecular weight of 710.2 and a CAS number of 2089251-47-6. The IUPAC name is heptadecan-9-yl 8-[2-hydroxyethyl-(6-oxo-6-undecoxyhexyl)amino]octanoate.


SM-102 can be synthesized through the route as shown in Figure 1.

Figure 1. Shows the synthesis route of SM-102.


SM-102 is an ideal drug carrier due to its fast clearance rate, tolerability, immunogenicity, and protein expression. While SM-102 is soluble in organic solvents, it forms a membrane when suspended in polar solvents. This property has enabled scientists to mold these lipids into mRNA therapeutics. SM-102 plays a significant role in the formulation of mRNA-1273. SM-102 remains neutral at physiological pH and takes on a positive charge in an acidic environment. This property to remain neutral at physiological pH allows the lipid to have fewer interactions with the anionic membranes of blood cells. SM-102's ability to take on a positive charge plays a crucial role after cellular uptake. When SM-102 interacts with the acidic endosome, it becomes protonated and forms cone-shaped ion pairs that drive the transition from a bilayer to an inverted hexagon phase. This phase promotes endosomal escape and the release of the mRNA into the cytosol. Once the mRNA is released, SM-102 is metabolized through ester hydrolysis, and the remaining aliphatic head group is eliminated via biliary and renal clearance.


With the recent advances in lipid technology, the scientific community is on the precipice of creating many new therapeutics. To further empower drug delivery research, BroadPharm offers a broad selection of ionizable lipids, cationic lipids, PEG lipids, and Phospholipids. BroadPharm also offers custom lipid syntheses to satisfy your research need.


Journal References

1.Han, X., Zhang, H., Butowska, K. et al. An ionizable lipid toolbox for RNA delivery. Nat Commun 12, 7233 (2021). doi.org/10.1038/s41467-021-27493-0

2.Hou, X., Zaks, T., Langer, R. et al. Lipid nanoparticles for mRNA delivery. Nat Rev Mater 6, 1078-1094 (2021).doi.org/10.1038/s41578-021-00358-0



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